Objective: The objective of the present study was to design and optimize oral fast dissolving film (OFDF) of practically insoluble drug lafutidine in order to enhance bioavailability and patient compliance especially for a geriatric and unconscious patient who are suffering from difficulty in swallowing.Methods: The films were prepared by a solvent casting method using low-grade hydroxyl propyl methyl cellulose (HPMC E5), polyvinyl alcohol (PVA), and sodium carboxymethyl cellulose (SCMC) as film forming polymers. Polyethylene glycol 400 (PEG400), propylene glycol (PG) and glycerin were used as a plasticizer to enhance the film forming properties of the polymer. Tween 80 (1% solution) and poloxamer407 were used as a surfactant, citric acid as a saliva stimulating agent, and croscarmellose as a super disintegrant. Films were then tested for both physical (weight variation, thickness, surface pH, drug content) and mechanical (folding endurance, tensile strength, percent elongation, Young's modulus) characteristics. In vitro disintegration, time and drug release profile were also determined for each formula.Results: Films were found to be satisfactory when evaluated for both physical and mechanical characterizations. The surface pH of all the films was found to be within the range of salivary pH 6.8. The USP dissolution apparatus type II (paddle type) was used for in vitro drug release studies. The optimized formulation F13 gave 100 % of drug released at 2 min. It also showed satisfactory surface pH (6.2±0.2), drug content (100.1±0.01%), the disintegration time of (7.0±0.5) seconds and the time needed for 80% of medication to be released (T80%) was 0.96 min.Conclusion: Lafutidine OFDF was formulated using HPMC E5 as film-forming a polymer with PEG400 as a plasticizer. Combination of tween80 (1% solution) and poloxamer407 as a surfactant were used in the presence of croscarmellose as a super disintegrant. The chosen OFDF disintegrates within seven seconds, releases the drug rapidly and gives an action.

Objective: The present study was aimed to develop a pH-triggered in situ gel for local release of lidocaine hydrochloride (lidocaine HCL) in the buccal cavity to improve the anesthetic effect of this amino amide drug which has very high water solubility. The formulations were introduced to the oral cavity as a spray to improve compliance and for easier administration.Methods: In this work, two grades of carbopol (934 and 940)-based in situ gel spray were designed. The formulations containing lidocaine HCl 5% were prepared by mixing different concentrations of carbopol with xanthan gum. Eight formulations were investigated and evaluated for gelation capacity, spray angle, volume of solution delivered per each actuation, rheological properties, and release kinetic model. Similarity factor (f2) was used for the comparison of dissolution profiles.Results: The prepared formulations undergo gelation after it had been actuated to the buccal cavity as a spray solution. The results showed that, as the concentration of polymer was increased, the release of drug decreased and the viscosity increased for both grades. The spray angle and volume of solution delivered per each actuation varied according to the composition of each formulation. The in situ gel containing 0.3% carbopol 934 and 0.2% xanthan gum regarded as a better candidate which had a good gelation and release property compared to other formulations. Drug release from optimized in situ gel spray followed Korsmeyer–Peppas model and was mediated by Fickian diffusion mechanism.Conclusion: Lidocaine HCl-loaded pH-sensitive in situ gel was successfully developed using carbopol 934 as polymer to be applied to the buccal cavity as spray solution for more effective anesthetic effect and painless treatment.

Flurbiprofen (FLB) is chemically 2-(3- fluoro-4-phenyl phenyl) propanoic acid. It is a nonsteroidal anti-inflammatory drug (NSAID) used in the treatment of rheumatoid arthritis and osteoarthritis. Oral administration of this drug is associated with severe gastrointestinal side effects like ulceration and gastrointestinal bleeding. The solution to this problem lies in the fact that topically applied NSAIDs are safer than orally. This study aims to prepare different topical semisolid formulation of FLB as cream base (o/w), (w/o) and gel base using different gel-forming agents in different concentrations. Comparing characterization properties in addition to release and diffusion study for all the prepared formulas to select the best one. Method: Topical semisolid FLB preparations were formulated using different semisolid formulation starting from emulsion bases w/o and o/w comparing with different gelling agents in different concentrations which include carbopol 934, sodium carboxy methylcellulose (SCMC) and combination of both polymer in different concentration to get 1% gelling agents. All the gel formulations were evaluated for physical appearance, pH, spreadability, rheological studies, drug content, in vitro release and diffusion studies. Results: All gel formulations which contain gelling agent exhibit better in vitro drug release and permeation compared with the emulsion bases, especially 1% polymer combination. Ethanol exerts a significant effect (p less than 0.05) on the in vitro drug release and diffusion for 2% carpbopol 934 compared with SCMC. Drug content was found to be uniform in all the formulations. The pH ranges of formulated gels were found to be suitable for topical application. Conclusion: Based on overall results, FLB can be successfully prepared as topical semisolid preparation with accepted properties.

Objective: Econazole nitrate (ECZ) is one of the triazole antifungal drugs with poor aqueous solubility and dissolution rate; there is a need for enhancement of solubility. Therefore; inclusion complexation with β cyclodextrin (βCD) was performed.Methods: In this study kneading method and co-evaporation method of preparation of inclusion complex between βCD and ECZ using two molar ratios of βCD. The solubility of these complexes in isotonic saline solution and distilled water was studied. Complexes prepared by kneading method were used for the preparation of different ophthalmic gel formulas using carbomer (CB) and sodium carboxymethylcellulose (sod CMC) as a gelling agent. The release profile and the rheological behaviour of the gel were studied.Results: The solubility of ECZ was enhanced by complexation with β CD, and both complexation methods showed Ap type solubility curve, but the solubility of ECZ was significantly enhanced by complexation using kneading method over co-evaporation. EZC-βCD complex prepared by kneading method with 0.88 *10-3 MβCD molar ratio and formulated in a gel using CB 0.75% w/w and sod CMC 0.25% w/w may be considered as a good candidate for ECZ ophthalmic gel dosage form, which showed Super case II transport release profile, and pseudo-plastic shear thinning behavior.Conclusion: Kneading method was found to be the best method for inclusion of ECZ into βCD, which significantly enhanced ECZ solubility; enabling to be formulated into an ophthalmic gel using CB as a polymer, for further development.

Attempts were made to improve solubility and the liquisolid technology dissolving of medication flurbiprofen. Liquisolid pill was developed utilizing transcutol-HP, polyethylene glycol 400, Avecil PH 102 carrier material and Aerosil 200 layer coating material. Suitable excipient amounts were determined to produce liquisolid powder using a mathematical model. On the other hand, flurbiprofen tablet with the identical composition, directly compressed, was manufactured for comparison without the addition of any unvolatile solvent. Both powder combination characterizations and after-compression tablets were evaluated. The pure drug and physical combination, and chosen liquisolid tablets were studied in order to exclude interacting with the differentional scanning calorimetry (DSC) and fourier transform infrared spectroscopy (FTIR). The results showed that transcutol is the ideal solvent with a solubility of 260±3.9 mg/ml in flurbiprofen. All formula developed were determined to be flowable within the specified limitations. The transcutol-like liquidsolid tablet formula of 35 percent w/w flurbiprofen and carrier to coating ratio of 10 was the most acceptable for the disintegration time, the tablet weight and other approved tablet characteristics. DSC thermographs demonstrated the development of a solid flurbiprofen amorphic solid solution for both the physical blend of the chosen liquisolid system and its tablets. The lack of chemicals interaction in medication and other components of the formula was demonstrated by the retention of all flurbiprofen characteristic peaks in all FTIR spectra. As an option to enhance solubility and dissolve flurbiprofen, which has a poor water solubility, liquisolid tablet has been evaluated.